BRD 7389P90 RSK inhibitor CAS# 376382-11-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 376382-11-5 | SDF | Download SDF |
| PubChem ID | 1080352 | Appearance | Powder |
| Formula | C24H18N2O2 | M.Wt | 366.41 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO | ||
| SMILES | C1=CC=C(C=C1)CCNC2=C3C4=CC=CC=C4C(=O)C5=C3C(=CC=C5)NC2=O | ||
| Standard InChIKey | XASCINRGTHLHGM-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C24H18N2O2/c27-23-17-10-5-4-9-16(17)21-20-18(23)11-6-12-19(20)26-24(28)22(21)25-14-13-15-7-2-1-3-8-15/h1-12,25H,13-14H2,(H,26,28) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Ribosomal S6 kinase (RSK) inhibitor (IC50 values are 1.2, 1.5 and 2.4 μM for RSK3, RSK1 and RSK2 respectively). Upregulates insulin expression in terminally differentiated pancreatic α-cells. |
BRD 7389 Dilution Calculator
BRD 7389 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7292 mL | 13.6459 mL | 27.2918 mL | 54.5837 mL | 68.2296 mL |
| 5 mM | 0.5458 mL | 2.7292 mL | 5.4584 mL | 10.9167 mL | 13.6459 mL |
| 10 mM | 0.2729 mL | 1.3646 mL | 2.7292 mL | 5.4584 mL | 6.823 mL |
| 50 mM | 0.0546 mL | 0.2729 mL | 0.5458 mL | 1.0917 mL | 1.3646 mL |
| 100 mM | 0.0273 mL | 0.1365 mL | 0.2729 mL | 0.5458 mL | 0.6823 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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BRD7389 is a Rsk family kinase inhibitor. [1]
Rsk has been suggested to phosphorylate a large number of cellular substrates and plays an important role in promoting cell growth and survival. Knockdown of Rsk family members would have an effect on insulin production inα-cells. Increasing in insulin expression upon RNAi of individual Rsk proteins can be observed, but the effect is not as strong as compound treatment with BRD7389.[1]
BRD7389 functions by inhibiting multiple Rsk family members simultaneously. BRD7389 also increases β-cell–specific gene expression in primary human islet cells. Assay-performance profile analysis suggests biochemical and cellular inhibition of the Rsk kinase family by BRD7389 is likely related to its ability induce a β-cell-like state. [2]
Treatment of TC1 cells with BRD7389 led to a decrease in the overall glycolytic activity and mitochondrial respiration rates, a phenotype reminiscent of the beta cell line. BRD7389 also increases the endocrine cell content and function of donor human pancreatic islets in culture.[2,3]
References:
[1]Sapkota GP, Cummings L, Newell FS,etal. , BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J. 2007 Jan 1;401(1):29-38.
[2]Choudhary A, Hu He K, Mertins P, etal. , Quantitative-proteomic comparison of alpha and Beta cells to uncover novel targets for lineage reprogramming. PLoS One. 2014 Apr 23;9(4):e95194.
[3]Fomina-Yadlin D, Kubicek S, Walpita D,etal. , Small-molecule inducers of insulin expression in pancreatic alpha-cells. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15099-104.
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